Pharmacokinetics and tissue tolerance of azithromycin after intramuscular administration to rabbits

Abstract The pharmacokinetics of azithromycin after intravenous and intramuscular injection at a single dose rate of 10 mg/kg bodyweight were investigated in rabbits by using a modified agar diffusion bioassay for determining plasma concentrations. The plasma creatine kinase activity was determined after i.m. administration for the evaluation of the tissue tolerance. The elimination half-lives of azithromycin after intravenous and intramuscular administration were 24.1 and 25.1 h, respectively. After intramuscular administration mean peak plasma concentration was 0.26 ± 0.01 mg/L and bioavailability was 97.7%. Plasma CK activity rose sharply within 8 h after i.m. injection of azithromycin; activity returned to pre-treatment level by 48–72 h post-treatment. The transient rise in serum CK activity indicates some degree of muscle tissue damage at the injection site.